合成目标产物 Carbamazepine 主要起始原料 Iminostilbene And Sodium Cyanate
(文献来源)合成步骤主要原料 Iminostilbene 和 Sodium Cyanate
5-氰基-5H-二苯并[b,F]氮杂卓置于硫酸,溶剂黄146体系中,用 Ice-Water 用作溶剂,化学反应生成卡马西平 参考文献:Process For The Production Of 5-Cyano-And 标题:Process For The Production Of 5-Cyano-And 摘要:该发明涉及一种新颖且技术先进的方法,通过在强极性物质存在下,将5H-二苯并[b,F]氮杂环庚烷与卤氰试剂反应制备5-氰基-5H-二苯并[b,F]氮杂环庚烷.5-氰基-5H-二苯并[b,F]氮杂环庚烷可用作制备5-羰基-10(11)-氧代-10,11-二氢-5H-二苯并[b,F]氮杂环庚烷的起始物质,该物质已知具有抑制中枢,抗抽搐和中枢肌肉松弛活性.
专利号:US-12264143-B2 优先权日:2020-12-17 标 题:Synthesis of cannabinoids and cannabinoid precursors, and related compounds, formulations, and methods of use 发明人:SAMMIS GLENN M; ROGGEN MARKUS 权利人:NALU BIO INC 摘要:Methods are provided for the synthesis of cannabinoids, including cannabidiol (CBD), cannabinol (CBN), cannabichromene (CBC), cannabidiolic acid (CBDA), cannabigerol (CBG), cannabigerolic acid (CBGA), cannabidivarin (CBDV), cannabidibutol (CBD-C4), dihydrocannabidiol (DCBD), tetrahydrocannabivarin (THCV), analogs thereof, and precursors to the foregoing. One method employs phloroglucinol or a phloroglucinol analog as a starting material. The syntheses are stereospecific, efficient, selective, and cost-effective, with little or no potential for generation of THC ((−)-trans-Δ9-tetrahydro-cannabinol) or any other psychoactive side product. Telescoped syntheses are also provided, as are new cannabinoids, pharmaceutical formulations, and methods of use.
专利号:US-9868752-B2 优先权日:2012-04-13 标题 :Modular assembly of metal-organic super-containers incorporating calixarenes 发明人:WANG ZHENQIANG; Dai feng-rong 权利人:UNIV OF SOUTH DAKOTA; SOUTH DAKOTA BOARD OF REGENTS 摘要:A new strategy to design container molecules is presented. Sulfonylcalix[4]arenes, which are synthetic macrocyclic containers, are used as building blocks that are combined with various metal ions and tricarboxylate ligands to construct metal-organic ‘super-containers’ (MOSCs). These MOSCs possess both endo and exo cavities and thus mimic the structure of viruses. The synthesis of MOSCs is highly modular, robust, and predictable.
专利号:US-12234200-B2 优先权日:2019-04-16 标 题:Synthetic methods of preparing esketamine 发明人:CHEN CHENG YI 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to methods for the asymmetric synthesis of esketamine. The present invention is further directed to key intermediates in the asymmetric esketamine synthesis. In one embodiment, the invention is an asymmetric synthesis of esketamine comprising the conversion of (S)-2′-chloro-2-methoxy-3,4,5,6-5 tetrahydro-[1, 1′-biphenyl]-3-yl carbamate to (S)-2′-chloro-1-isocyanato-6-methoxy-1,2,3,4-tetrahydro-1,1′-biphenyl.
专利号:US-7576211-B2 优先权日:2004-09-30 标题 :Synthesis of thienopyridinone compounds and related intermediates 发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE 权利人:EPIX DELAWARE INC 摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
专利号:US-2022233673-A1 优先权日:2019-06-04 标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF 发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M 权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND 摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.
专利号:WO-2016111658-A1 优先权日:2015-01-07 标 题:Synthesis of thiosemicarbazone derivatives comprising sulphonamide group with potential anticonvulsant activity 发明人:IYIDOGAN AYSEGUL; EMRE EMINE ELCIN; TOPALFAKIOGÄžLU RAHIME BETÜL; KAYMAKÇIOÄžLU BEDIA; ARICIOÄžLU FEYZA 权利人:IYIDOGAN AYSEGUL; EMRE EMINE ELCIN 摘要:The present invention relates to the synthesis method of thiosemicarbazone derivatives comprising sulphonamide group and having high anticonvulsant/antiepileptic activity.
1: Xiao Y, Gan L, Wang J, Luo M, Luo H. Vigabatrin versus carbamazepine monotherapy for epilepsy. Cochrane Database Syst Rev. 2015 Nov 18;11:CD008781. [Epub ahead of print] Review. pii: bcr2015211439. doi: 10.1136/bcr-2015-211439. doi: 10.1016/S0034-7450(14)60011-1. Epub 2014 May 10. Review. Spanish. 4β-Hydroxycholesterol correlates with dose but not steady-state concentration of carbamazepine: indication of intestinal CYP3A in biomarker formation? Br J Clin Pharmacol. 2015 Nov 17. doi: 10.1111/bcp.12833. [Epub ahead of print]
合成参考文献
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